Proconvulsant and ‘anxiogenic’ effects of n-butyl β carboline-3-carboxylate, an endogenous benzodiazepine binding inhibitor from brain

Novas, M.L.; Wolfman, Claudia; Medina, Jorge H.; Robertis, E. De

doi:10.1016/0091-3057(88)90463-7

Cited by 87 publications

(33 citation statements)

References 8 publications

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“…In this way, we decided to study the effects of riparin III in the open field test, a classical animal model that allows measurements through which is possible to evaluate autonomic effects of drugs and general activity of animals. 30) Our findings show that riparin III (25, 50 mg/kg) did not alter the locomotor activity different from diazepam 2 mg/kg which decreased this parameter showing a sedative effect. Likewise, it is unlikely that these effects of riparin III observed in the plus maze and hole board tests are based on the stimulation of general motor activity.…”

Section: Discussionmentioning

confidence: 56%

Anxiolytic-Like Effects of (O-Methyl)-N-2,6-dihydroxybenzoyl-tyramine (Riparin III) from Aniba riparia (NEES) MEZ (Lauraceae) in Mice

Melo

Monteiro

Leite

et al. 2006

Biological & Pharmaceutical Bulletin

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Section: Discussionmentioning

confidence: 56%

Anxiolytic-Like Effects of (O-Methyl)-N-2,6-dihydroxybenzoyl-tyramine (Riparin III) from Aniba riparia (NEES) MEZ (Lauraceae) in Mice

Melo

Monteiro

Leite

et al. 2006

Biological & Pharmaceutical Bulletin

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“…24) Our findings show that the animals treated with riparin II (25, 50, 75 mg/kg) did not alter the locomotor activity, different from diazepam (2 mg/kg) which decreased this parameter showing a sedative effect. In addition, the anxiolytic-like effect of riparin II seems not to be associated with any motor effects since it did not alter significantly the ambulatory behavior in the open field test.…”

Section: Discussionmentioning

confidence: 60%

Evaluation of Effects of N-(2-Hydroxybenzoyl) Tyramine (Riparin II) from Aniba riparia (NEES) MEZ (Lauracea) in Anxiety Models in Mice

Sousa

Leite

Melo

et al. 2007

Biological & Pharmaceutical Bulletin

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Aniba riparia (NEES) MEZ, from the Lauraceae family, is popularly named "louro" in Brazil. It belongs to a genus mainly found in Central Amazonia and Guiana comprising approximately 40 species of lowland shrubs and trees. 1,2) From the green fruit of Aniba riparia, collected from the Amazonas state of Brazil, were isolated three substances with broad spectrum antimicrobial activity: methyl ethers of N-benzoyl tyramine (riparin I), N-(2-hydroxybenzoyl) tyramine (riparin II) and N-(2,6-dihydroxybenzoyl) tyramine (riparin III) 1) which were later synthesized.3)It was previously reported that (O-methyl)-N-(2,6-dihydroxybenzoyl) tyramine (riparin III) has potent smooth muscle relaxant activity 4,5) and this spasmolytic effect was possibly related to a reduction of intracellular Ca 2ϩ concentration. 6)Recently, it was reported by us that riparin I 7) and III 8,9) presented antianxiety effects in mice treated with the doses of 25 and 50 mg/kg. As far as we know, there are no studies in the literature on the central actions of riparin II. However, this substance is an N-(2-hydroxybenzoyl) tyramine, and previous data showed that the spectrum of tyramine actions are similar to those of norepinephrine. In fact, some reports related that tyramine-rich foods when ingested by individuals taking antidepressant drugs, such as monoamino oxidase inhibitors, might result in a prolonged increase in blood pressure. 10)Hereby, these findings led us to investigate the behavioral effects of riparin II on animals models of locomotion, anxiolytic and myorelaxant activities. MATERIALS AND METHODS AnimalsMale Swiss mice weighing 25-30 g were used in these experiments. The animals were housed in plastic cages, 30 to cage, under a 12 h light/dark cycle (light on at 7:00 a.m.) at constant temperature of 23Ϯ1°C with free access to food and water, except during the experiments. Animals were treated in accordance to the current law and the NIH Guide for Care and Use of Laboratory Animals.Drugs Riparin II was emulsified with 3% Tween 80 (Sigma-U.S.A.) and dissolved in distilled water. Animals were treated with the compound in doses of 25, 50 and 75 mg/kg, once, 30 or 60 min before the experiments when administered by intraperitoneal or oral routes, respectively. Controls received vehicle at the same volume (10 ml/kg) and the same route as the treated groups. Diazepam (DZP), União Química Brazil, (1, 2 mg/kg) was used as standard.Experimental Protocol The animals were tested during the light period and were observed in a closed room at constant temperature (23Ϯ1°C) and poorly illuminated with a 15-V red light. One hour after the treatment, the open field and rota rod tests were performed with the same animals in the manner described below: Firstly, the animal was placed in the open field area for 5 min. Immediately after the open field test, the animal was removed to the rota rod where it was evaluated for 1 min. All the other tests were performed in different days with other groups of animals. Physiology and Pharmacology, Faculty of Medicine, Fe...

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“…Alterations in the production and or release of an endogenous ligand for the benzodiazepine receptor with inverse agonist properties have been postulated as a mechanism for the occurrence of the tolerance/withdrawal phenomena (Baldwin & File, 1988). Interestingly, the presence of endogenous n-butyl 13 carboline-3-carboxylate, which possesses inverse agonist properties, has indeed been demonstrated (Novas et al, 1988;Medina et al, 1989). In man also, the occurrence of tolerance/withdrawal phenomena with regard to the pharmacological effects of benzodiazepines appears to be ubiquitous (Bliding, 1974;Greenblatt et al, 1977;1981;Macleod et al, 1977;Greenblatt & Shader, 1978;Ellinwood et al, 1983;1985;1987;Salzman et al, 1983;Ashton et al, 1988).…”

Section: Discussionmentioning

confidence: 99%

Pharmacodynamics of the anticonvulsant effect of oxazepam in aging BN/BiRij rats

Stijnen

Postel-Westra

Langemeijer

et al. 1992

British J Pharmacology

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Proconvulsant and ‘anxiogenic’ effects of n-butyl β carboline-3-carboxylate, an endogenous benzodiazepine binding inhibitor from brain

Cited by 87 publications

References 8 publications

Anxiolytic-Like Effects of (O-Methyl)-N-2,6-dihydroxybenzoyl-tyramine (Riparin III) from Aniba riparia (NEES) MEZ (Lauraceae) in Mice

Anxiolytic-Like Effects of (O-Methyl)-N-2,6-dihydroxybenzoyl-tyramine (Riparin III) from Aniba riparia (NEES) MEZ (Lauraceae) in Mice

Evaluation of Effects of N-(2-Hydroxybenzoyl) Tyramine (Riparin II) from Aniba riparia (NEES) MEZ (Lauracea) in Anxiety Models in Mice

Pharmacodynamics of the anticonvulsant effect of oxazepam in aging BN/BiRij rats

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